MK-6884
目录号: PL06818 纯度: ≥99%
CAS No. :2102194-04-5
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中文名称
MK-6884
英文名称
MK-6884
英文别名
2-Pyridinecarbonitrile, 6-(2,3-dihydro-2-methyl-3-oxo-1H-isoindol-5-yl)-5-[1-[(1-methylcyclopentyl)methyl]-1H-pyrazol-4-yl]-;MK-6884;CS-0369341;6-(2-methyl-3-oxo-2,3-dihydro-1H-isoindol-5-yl)-5-{1-[(1-methylcyclopentyl)methyl]-1H-pyrazol-4-yl}pyridine-2-carbonitrile;AKOS040757290;HY-141899;EN300-7544928;GLXC-25181;EX-A6079;2102194-04-5;6-(2-Methyl-3-oxoisoindolin-5-yl)-5-(1-((1-methylcyclopentyl)methyl)-1H-pyrazol-4-yl)picolinonitrile;MS-27105;SCHEMBL19031979
Cas No.
2102194-04-5
分子式
C25H25N5O
分子量
411.50
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
MK-6884 是一种 M4 毒蕈碱受体正变构调节剂 (PAM),其 Ki 值为 0.19 nM。MK-6884 可用于神经退行性疾病的研究。MK-6884 可用 11C 放射标记作为正电子发射计算机断层扫描显像剂。
生物活性
MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a K i value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent.
性状
Solid
IC50 & Target[1][2]
mAChR4
体外研究(In Vitro)
MK-6884 (compound 13; 0-22 μM) is a PAM of ACh function in a cell-based Ca mobilization assay, with an EC50 of 27 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
[C]MK-6884 (compound 13) shows non-displaceable binding potential (BP ND ) of 0.83 in rhesus monkeys.
[C]MK-6884 (approximately 185 MBq, <2 μg; single intravenous) distributes on the known presence of M4 receptors in the rhesus monkeys brain.
[C]MK-688 can penetrate the blood-brain barrier in monkeys. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Tong L, et al. Discovery of [C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases. J Med Chem. 2020;63(5):2411-2425.
溶解度数据
In Vitro: THF : 3.33 mg/mL (8.09 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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